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(+)-Bicuculline Sale

(Synonyms: (+)-荷包牡丹碱,Bucuculline) 目录号 : GN10745

A GABAA receptor antagonist

(+)-Bicuculline Chemical Structure

Cas No.:485-49-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥539.00
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50mg
¥378.00
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250mg
¥1,397.00
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Primary cortical neurons from rat E18 embryos

Preparation method

The solubility of this compound in DMSO >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM for 15–60 min

Applications

Bicuculline treatment could potentiate synaptic NMDAR signaling in the primary cortical neurons. Bicuculline led to a rapid decrease in STEP61 expression and a concomitant increase in the tyrosine phosphorylation of STEP substrates including GluN2B, Pyk2, and ERK1/2.

Animal experiment [2]:

Animal models

13-month old Fischer- 344 virgin female ovariectomized rats.

Dosage form

3.5 mg/kg( dissolved in sesame oil + 10% DMSO) daily by injection for 26 days

Application

The GABAA antagonist bicuculline attenuated progesterone-induced memory impairments in middle-aged ovariectomized rats.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Xu J1, Kurup P1, et al, Synaptic NMDA Receptor Activation Induces Ubiquitination and Degradation of STEP61. Mol Neurobiol. 2017 May 2. doi: 10.1007/s12035-017-0555-x.

[2] Braden BB1, Kingston ML, et al, The GABAA antagonist bicuculline attenuates progesterone-induced memory impairments in middle-aged ovariectomized rats. Front Aging Neurosci. 2015 Aug 14;7:149. doi: 10.3389/fnagi.2015.00149. eCollection 2015.

产品描述

(+)-Bicuculline is a light-sensitive competitive antagonist of GABA-A receptor.

References:
[1]. Zahm DS, et al. Comparison of the locomotor-activating effects of bicuculline infusions into the preoptic area and ventral pallidum. Brain Struct Funct. 2014 Mar;219(2):511-26.
[2]. Johnston GA. Advantages of an antagonist: bicuculline and other GABA antagonists. Br J Pharmacol. 2013 May;169(2):328-36.

Chemical Properties

Cas No. 485-49-4 SDF
别名 (+)-荷包牡丹碱,Bucuculline
化学名 (6R)-6-[(5S)-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-5-yl]-6H-furo[3,4-g][1,3]benzodioxol-8-one
Canonical SMILES CN1CCC2=CC3=C(C=C2C1C4C5=C(C6=C(C=C5)OCO6)C(=O)O4)OCO3
分子式 C20H17NO6 分子量 367.11
溶解度 ≥ 13.1mg/mL in DMSO 储存条件 Store at -20°C, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.724 mL 13.6199 mL 27.2398 mL
5 mM 0.5448 mL 2.724 mL 5.448 mL
10 mM 0.2724 mL 1.362 mL 2.724 mL
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